Exploring solid form 0 of Clarithromycin

Conferencia; 6ta Reunión Internacional de Ciencias Farmacéuticas (RICiFa)-Edición Aniversario 10 años-; 2021

Some polymorphic drugs may undergo solid-state transformations during productionand/or storage processes, which are a problem in their performance characteristics affecting themechanical and physical drug properties, such as solubility and stability. Therefore, a profoundcharacterization to identify each solid form of a drug is essential to monitor any physical transitionutilizing quality control techniques. The present study was conducted as a strategy to provideinformation on solid form 0 of clarithromycin, an ethanol solvate. The structural characterization wascarried using a variety of techniques, such as solid state nuclear magnetic resonance, X-ray powderdiffraction, infrared spectroscopy, thermo analytical methods and confocal microscopy. In addition,solubility, stability and microbiological studies were performed. These studies showed characteristicpatterns and morphological particularities, which allowed the unequivocal identification of this solidform. Interestingly, the solid showed good antimicrobial activity, altough it is less soluble than theform II currently used on the market. The physical stability under normal storage conditions revealeda desolvation process and a subtle polymorphic transformation. Therefore, the properties determinedin our study, represent specific data that could be useful tools to recognize aspects in routinelaboratory testing of quality control to ensure that the solid form used remains stable in the finaltherapeutic dosage form.